lepirudin

Lepirudin is a recombinant form of hirudin, a naturally occurring anticoagulant originally derived from the medicinal leech *Hirudo medicinalis*. It is produced in yeast cells and differs from natural hirudin by a single amino acid substitution (leucine for isoleucine at the N-terminus) and the absence of a sulfate group on tyrosine at position 63[3][5]. Lepirudin acts as a highly specific direct thrombin inhibitor by binding irreversibly to both free and clot-bound thrombin at its catalytic and substrate-binding sites. This action blocks thrombin’s protease activity, thereby inhibiting fibrin formation and preventing blood coagulation[1][2][3]. Unlike heparin, its effect does not depend on antithrombin III and it is not inhibited by platelet factor 4. Lepirudin was primarily indicated for anticoagulation in patients with heparin-induced thrombocytopenia (HIT), especially when heparins are contraindicated due to HIT or associated thromboembolic disease[1][3][5]. The drug is eliminated mainly via the kidneys.

Brand names

Refludan

Other names

lepirudin rDNA for injectionrecombinant hirudin[Leu1, Thr2]-63-desulfohirudin